o-Phenanthroline is a commonly used organic chelating agent and ligand that can form stable complexes with a variety of metal ions (such as Fe²⁺, Zn²⁺) [1]. o-Phenanthroline forms a red-orange complex with Fe²⁺, with a maximum absorption wavelength of about 510nm [2]. o-Phenanthroline is also an important broad-spectrum inhibitor of matrix metalloproteinases (MMPs). Its mechanism of action is to inhibit the enzymatic activity of MMP by chelating the metal ions (such as Zn²⁺) in the active center of MMP [3-4].
In human umbilical vein endothelial cells o-Phenanthroline (0.3mM; 24h) had some cytotoxicity to the cells, and the level of MMP-2 detected in gelatin zymography was decreased [5]. In cultured endothelial cells exposed to the enzyme reaction hypoxanthine-xanthine oxidase (HX-XO) or pure H2O2, O-phenanthroline (100μM; 15min) afforded a complete protective effect against DNA strand breakage and the associated activation of the enzyme poly(ADP) ribose polymerase [6]. In Human primary chondrocytes, the upregulation of HIF1α expression in cells treated with O-Phenanthroline (2-5μM; 10h) [7].
In BALB/c mice, hematopoietic stem/progenitor cells mobilization was significantly inhibited by o-Phenanthroline (100mg/kg; ip; 3d) [6].
References:
[1]. Mu G N, Li X, Li F. Synergistic inhibition between o-phenanthroline and chloride ion on cold rolled steel corrosion in phosphoric acid[J]. Materials Chemistry and Physics, 2004, 86(1): 59-68.
[2]. Liu C, Liu Q, Lv Y, et al. CPLX1 is a novel prognostic biomarker in CRC correlating with immunotherapy resistance and ferroptosis[J]. Frontiers in Immunology, 2025, 16: 1589423.
[3]. Liu ZiQiang, Liu YuXin, Zhou DaYong, et al. The role of matrix metalloprotease (MMP) to the autolysis of sea cucumber (Stichopus japonicus)[J]. 2019.
[4]. Kato Y, Yamashita T, Ishikawa M. Relationship between expression of matrix metalloproteinase-2 and matrix metalloproteinase-9 and invasion ability of cervical cancer cells[J]. Oncology reports, 2002, 9(3): 565-569.
[5]. Lafleur M A, Hollenberg M D, Atkinson S J, et al. Activation of pro-(matrix metalloproteinase-2)(pro-MMP-2) by thrombin is membrane-type-MMP-dependent in human umbilical vein endothelial cells and generates a distinct 63 kDa active species[J]. Biochemical Journal, 2001, 357(1): 107-115.
[6]. Jin F, Zhai Q, Qiu L, et al. Degradation of BM SDF-1 by MMP-9: the role in G-CSF-induced hematopoietic stem/progenitor cell mobilization[J]. Bone marrow transplantation, 2008, 42(9): 581-588.
[7]. Georgi N, Landman E B M, Klein T J, et al. O‐Phenanthroline as modulator of the hypoxic and catabolic response in cartilage tissue‐engineering models[J]. Journal of tissue engineering and regenerative medicine, 2017, 11(3): 724-732.
o-Phenanthroline是一种常用的有机螯合剂和配体，能与多种金属离子（如Fe²⁺、Zn²⁺）形成稳定的配合物 [1]。o-Phenanthroline与Fe²⁺形成橙红色配合物，最大吸收波长约为510nm [2]。o-Phenanthroline也是一种重要的基质金属蛋白酶（MMP）广谱抑制剂，其作用机制是通过螯合MMP活性中心的金属离子（如Zn²⁺）来抑制MMP的酶活性 [3-4]。
在人脐静脉内皮细胞中，o-Phenanthroline（0.3mM；24h）对细胞有一定的细胞毒性，明胶酶谱法检测的MMP-2水平降低 [5]。在培养的内皮细胞中，暴露于次黄嘌呤-黄嘌呤氧化酶（HX-XO）或纯H2O2的酶反应中，o-Phenanthroline（100μM；15min）可完全保护内皮细胞免受DNA链断裂及其相关的聚（ADP）核糖聚合酶的激活 [6]。在人原代软骨细胞中，用o-Phenanthroline（2-5μM；10h）处理的细胞中HIF1α表达上调 [7]。
在BALB/c小鼠中，c（100mg/kg；ip；3d）显著抑制造血干细胞/祖细胞的动员 [6]。